GDC-0941 is a highly potent and selective class I PI3K kinase inhibitor under development. Its IC50 values for for PI3K p110 α, β, δ and γ isoforms are 3nM, 33nM, 3nM, 75nM, and for DNA-PK and mTOR are 1230nM and 580nM. It is now in phase I clinical trials targeting several advanced or metastatic solid tumors.
Technical information:
| Chemical Formula: | C23H27N7O3S2 | |
| CAS #: | 957054-30-7 | |
| Molecular Weight: | 513.64 | |
| Purity: | >98% | |
| Appearance: | White solid | |
| Chemical Name: | 4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine | |
| Solubility: | Up to 100 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | AJ Folkes et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J. Med. Chem. 2008, 51(18), 5522-32. |
| 2. | FI Raynaud et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol. Cancer Ther. 2009, 8(7), 1725-38. |
| 3. | Zheng L, et al. GDC-0941 sensitizes breast cancer to ABT-737 in vitro and in vivo through promoting the degradation of Mcl-1.Cancer Lett. 2011;309(1):27-36. |
Other Information:
Product Specification (pdf)MSDS (pdf)
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